Euticals Spa

Hoffmann-la Roche Inc.

Boehringer Ingelheim International Gmbh

F. Hoffmann-la Roche Ag

Torsten Busch

Michael Nonnenmacher

Markus Ostermeier

Joerg Jung

Sven Anklam

The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters thereof of formula (I) in high yields starting from a dialkyl ketal derivative of formula (V) 

Process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters

The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters thereof of formula (I) in high yield. The claimed process uses diarylketal formula (V) to generate an arylbromide of formula (III) in which the amino-group is protected as bisarylmethylidenimino-group, which is then transformed into a formula (I) compound. 

Disclosed is a method for the synthesis of spiro[2.5]octane-5,7-dione useful as intermediate in the manufacture of pharmaceutically active ingredients. Also disclosed are novel intermediates used in the synthesis of this compound.

Process for preparing spiro[2.5]octane-5,7-dione

The present invention relates to a process for the preparation of 2-amino-pyrimidine-5-boronic acid of formula (I). 

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Frankfurt am Main, Germany

Torsten Busch